The Cu-catalyzed version of the classic Huisgen azide-alkyne cycloaddition is a highly atom-economical reaction, often requiring mild conditions. Both factors render Cu-catalyzed azide-alkyne cycloaddition (CuAAC) highly attractive for the modification of complex and sensitive molecules such as nucleosides. Thus, such a method can be readily applied for the modification of nucleosides. Nucleosides are a highly important class of biomolecules, with applications in biochemistry, biology, as biological probes, and in medicine. O6-protected 2-azidoinosine derivatives and their 2′-deoxyinosine analogues are potentially very useful intermediates for use in CuAAC reactions. C-2 (1,2,3-triazol-1H-yl)inosine and 2′-deoxyinosine analogues can be synthesized by O6-benzotriazolyl derivatives, and these can be further converted to C-2 (1,2,3-triazol-1H-yl)adenosine analogues. Both classes of compounds are anticipated to have high importance in the fields of biochemistry, biology, and medicine.